Novel Chelating Agents for Zirconium-89-Positron Emission Tomography (PET) Imaging: Synthesis, DFT Calculation, Radiolabeling, and In Vitro and In Vivo Complex Stability.

ABSTRACT: We report the synthesis and evaluation of novel chelating agents for zirconium-89 (⁸⁹Zr) with positron emission tomography (PET) imaging applications. New chelating agents NODHA, NOTHA, and NODHA-PY were constructed on 1,4,7-triazacyclononane (TACN) and possess hydroxamic acid or a pyridine ring as an acyclic binding moiety. The new chelating agents were theoretically studied for complexation with Zr(IV). Structures of Zr(IV)-NODHA, Zr(IV)-NOTHA, and Zr(IV)-NODHA-PY were predicted using density functional methods. NODHA was found to form stronger bonds with Zr(IV) when compared to NOTHA and NODHA-PY. The new chelating agents were evaluated for radiolabeling efficiency in binding ⁸⁹Zr. The corresponding [⁸⁹Zr]Zr-labeled chelators were evaluated for complex s

SUBMITTER: Kang CS 

PROVIDER: S-EPMC9607665 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature